Third Generation Egfr Inhibitors: Overcoming Egfr Resistance And Toxicity Problems

EGFR inhibitors are useful tools in cancer therapeutics, but resistance to the first generations have significantly increased, meaning a new generation of improved inhibitors are needed with better efficacy and lower toxicity. Third Generation EGFR Inhibitors: Overcoming EGFR Resistance and Toxicity Problems reviews current issues relating to the design of reversible and irreversible third generation EGFR inhibitors, highlighting the types of mutation responsible for resistance, and providing different chemical starting points for researchers to optimize and develop in designing the next generation of drugs. Beginning with an introduction to EGFR inhibitors and a review of inhibitors currently approved or in clinical trials, the book goes on to discuss current approaches in the development of both covalent irreversible and covalent reversible EGFR Inhibitors. Mechanisms of resistance to third generation inhibitors, and discovery of fourth generation allosteric C797S inhibitors are then explored before a discussion of potential future trends. Third Generation EGFR Inhibitors: Overcoming EGFR Resistance and Toxicity Problems is a guide for medicinal chemists, drug developer, and researchers investigating cancer therapeutics, supporting them in the design and development of improved analogues to overcome the problems of resistance and toxicity associated with third generation EGFR inhibitors. Includes full synthetic schemes of all approved and in-trial third generation inhibitors Highlights the emergence of fourth generation EGFR inhibitors and looks at how they may be able to overcome the constraints of third generation compounds Provides a structural correlation of third and fourth generation EGFR inhibitors and reviews both their design strategies and typical anticancer activity

• | Author: Harun M. Patel, Rahul Pawara, S. J. Surana
• | Publisher: Elsevier
• | Publication Date: Dec 03, 2018
• | Number of Pages: 290 pages
• | Language: English
• | Binding: Paperback/Medical
• | ISBN-10: 0081026617
• | ISBN-13: 9780081026618